Technical Specification: Small Molecule Compounds¶
1. Product Description¶
Solarbio small molecule compounds include signaling pathway modulators, enzyme inhibitors, receptor agonists/antagonists, ion channel blockers, fluorescent probes, and chemical biology tools. Each compound is supplied with a Certificate of Analysis documenting purity by HPLC or GC, identity by NMR and MS, and physical characterization data.
2. Complete Product Categories and Examples¶
| Category | Example Compounds | Target/Pathway | Primary Application |
|---|---|---|---|
| Kinase Inhibitors | SB203580, PD98059, LY294002, U0126, SP600125, Ruxolitinib, Gefitinib, Dasatinib | p38 MAPK, MEK1/2, PI3K/Akt, JNK, JAK/STAT, EGFR, Src | Cell signaling, cancer research |
| PI3K/Akt/mTOR | Rapamycin, Wortmannin, GDC-0941, MK-2206, AZD8055, Torin 1, BEZ235 | mTOR, PI3K, Akt, mTORC1/C2 | Autophagy, proliferation, metabolism |
| Apoptosis Inducers | Staurosporine, Etoposide, Camptothecin, Doxorubicin, Cisplatin, ABT-737, Venetoclax | Topoisomerase I/II, PKC, DNA intercalation, Bcl-2 | Cell death mechanisms, oncology |
| NF-κB Pathway | BAY 11-7082, MG-132, Parthenolide, PDTC, Triptolide, Celastrol, Curcumin | IKK, 20S proteasome, NF-κB translocation | Inflammation, immunity, cancer |
| Antioxidants | N-Acetyl-L-cysteine (NAC), Trolox, Resveratrol, Tempol, MnTBAP, Ebselen, GSH-monoester | ROS scavenging, SOD mimetic, GPx mimetic | Oxidative stress, neuroprotection |
| Epigenetic Modulators | Trichostatin A (TSA), SAHA (Vorinostat), 5-Aza-2′-deoxycytidine, GSK-J4, UNC1999, JQ-1, RGFP966 | HDAC, DNMT, JMJD3, EZH2, BET bromodomain, HDAC3 | Epigenetics, chromatin biology, differentiation |
| Antibiotics | Puromycin, Blasticidin S, Geneticin (G418), Hygromycin B, Cycloheximide, Actinomycin D, Zeocin | Protein synthesis (ribosome), transcription (RNA pol), selection markers | Stable cell line selection, translation studies |
| Autophagy Modulators | Rapamycin, Chloroquine, 3-Methyladenine, Torin 1, Bafilomycin A1, Spautin-1, Metformin | mTOR, lysosomal pH, PI3K class III, V-ATPase | Autophagy flux analysis, metabolic diseases |
| Natural Products | Curcumin, Quercetin, Berberine, Resveratrol, Epigallocatechin gallate (EGCG), Baicalein, Ginkgolide B | Multiple targets (NF-κB, PI3K, AMPK, HDAC) | Broad biological activity, herbal pharmacology |
| Fluorescent Probes | DCFH-DA, DHE, Fluo-4 AM, JC-1, Rhodamine 123, Hoechst 33342, MitoTracker Red | ROS, Ca²⁺, MMP, DNA, mitochondria | Live-cell imaging, flow cytometry |
| Ion Channel Modulators | Verapamil, Nifedipine, 4-AP, TEA, Amiloride, Capsaicin, Tetrodotoxin | Ca²⁺ (L-type), K⁺ (voltage-gated), Na⁺ (epithelial, voltage-gated), TRPV1 | Electrophysiology, cardiac research |
| Lipid Signaling Modulators | Arachidonic acid, GW9662, WY-14643, Rosiglitazone, AICAR, Compound C, GW501516 | PPARγ, PPARα, AMPK, COX-2 | Metabolic research, lipid biology |
3. Solubility Reference Table¶
| Compound Category | DMSO | Ethanol (≥95%) | Water | PBS (pH 7.4) | Recommended Stock Solvent |
|---|---|---|---|---|---|
| Kinase inhibitors | 30–100 mM | 5–20 mM | <1 mM | <1 mM | DMSO |
| PI3K/mTOR inhibitors | 10–100 mM | 2–10 mM | <0.1 mM | <0.1 mM | DMSO |
| Apoptosis inducers | 10–50 mM | 5–40 mM | <5 mM (cisplatin: 5 mg/mL) | <5 mM | DMSO or water (cisplatin) |
| HDAC inhibitors (TSA, SAHA) | 20–50 mM (TSA); 50–100 mM (SAHA) | 10–20 mM | 1–5 mM (TSA); 10–20 mM (SAHA) | 5–10 mM (SAHA) | DMSO or ethanol |
| DNMT inhibitors | 10–40 mM | 5–10 mM | 5–20 mM | 5–20 mM | DMSO or water |
| BET inhibitors (JQ-1) | 20–50 mM | 5–15 mM | <0.1 mM | <0.1 mM | DMSO |
| Antibiotics | 50–100 mM | 10–50 mM | 10–50 mg/mL | 10–50 mg/mL | Water (most), DMSO (some) |
| Antioxidants (NAC) | 100–500 mM | 20–100 mM | 50–200 mM | 50–200 mM | Water |
| Natural products | 10–50 mM | 5–20 mM | <1 mM | <1 mM | DMSO or ethanol |
| Fluorescent probes | 1–20 mM | 1–5 mM | <0.1 mM | <0.1 mM | DMSO (anhydrous) |
| Ion channel blockers | 10–100 mM | 5–30 mM | 1–20 mM | 1–20 mM | DMSO or water (verapamil) |
| Lipid modulators | 20–100 mM | 10–50 mM | <0.1 mM | <0.1 mM | DMSO or ethanol |
Note: Solubility values are approximate at 25°C. For insoluble compounds, sonication (30 s at 40 kHz) or gentle warming (37°C, 5 min) may improve dissolution. Do not exceed 50°C for heat-sensitive compounds.
4. Cell-Based Assay Recommendations¶
| Compound Category | Recommended Cell Lines | Standard Assay Duration | Typical Endpoint |
|---|---|---|---|
| Kinase inhibitors | HEK-293, HeLa, A549, MCF-7, HCT-116 | 24–72 h | Phospho-specific western blot, MTT, Caspase-3 |
| PI3K/mTOR inhibitors | MCF-7, PC-3, U87MG, HEK-293T | 24–72 h | p-Akt (Ser473) by WB, proliferation (BrdU/EdU) |
| Apoptosis inducers | HeLa, Jurkat, HL-60, K562, U-937 | 12–48 h | Annexin V/PI flow cytometry, caspase activity |
| Epigenetic modulators | HEK-293, HeLa, K562, MCF-7, HCT-116 | 24–72 h | Histone acetylation (Ac-H3, Ac-H4) by WB, ChIP-qPCR |
| Antibiotics (selection) | HEK-293, CHO-K1, HeLa, SH-SY5Y | 7–14 days | Colony formation, viability (IC₅₀ determination) |
| Autophagy modulators | HeLa, HEK-293, MEF, SH-SY5Y | 6–24 h | LC3-II/LC3-I ratio by WB, GFP-LC3 puncta (microscopy) |
| Antioxidants | SH-SY5Y, HepG2, RAW 264.7, H9c2 | 1–24 h (pretreatment + stress) | ROS levels (DCFH-DA flow cytometry), MTT |
| Natural products | HeLa, A549, HepG2, Caco-2, RAW 264.7 | 24–72 h | Cell viability (MTT/WST-1), ROS, pro-inflammatory cytokines |
| Fluorescent probes | Any adherent suspension cell line | 15–60 min (loading) + 1–60 min (imaging) | Fluorescence microscopy (live-cell), flow cytometry |
| Ion channel blockers | SH-SY5Y, PC-12, HEK-293 (transfected), primary neurons | 5–30 min (acute), 24–48 h (chronic) | Patch-clamp, calcium imaging (Fluo-4), membrane potential |
5. IC₅₀ Reference Ranges from Literature¶
| Compound | Target | Reported IC₅₀ Range | Cell-Free IC₅₀ | Cell-Based IC₅₀ |
|---|---|---|---|---|
| SB203580 | p38 MAPK | 0.3–0.6 µM | 0.3–0.5 µM | 0.5–10 µM |
| PD98059 | MEK1 | 2–10 µM | 4 µM | 10–50 µM |
| LY294002 | PI3K (p110α/β/δ) | 0.5–1.4 µM | 1.4 µM (PI3K p110α) | 5–25 µM |
| U0126 | MEK1/2 | 0.07–0.5 µM | 0.07 µM (MEK1), 0.06 µM (MEK2) | 5–20 µM |
| Rapamycin | mTORC1 | 0.1–10 nM | 0.1 nM | 10–100 nM |
| Staurosporine | PKC (pan) | 1–50 nM | 2–10 nM (PKC), 1–3 nM (cAMP/PKA) | 5–100 nM |
| Trichostatin A (TSA) | HDAC1/2/3/6 | 1–20 nM | 2 nM (HDAC1), 4 nM (HDAC6) | 10–200 nM |
| SAHA (Vorinostat) | HDAC1/2/3/6 | 20–100 nM | 30 nM (HDAC1), 40 nM (HDAC3) | 0.5–5 µM |
| 5-Aza-2′-deoxycytidine | DNMT1 | 0.1–2 µM | 0.5 µM | 0.1–5 µM |
| JQ-1 | BRD4 | 20–100 nM | 50 nM (BRD4 BD1), 90 nM (BD2) | 0.1–1 µM |
| Puromycin | 60S ribosome | 0.5–5 µg/mL | 1–2 µg/mL (in vitro translation) | 0.5–10 µg/mL |
| Chloroquine | Lysosomal pH | 10–50 µM | — | 10–100 µM |
| N-Acetyl-L-cysteine | ROS scavenger | 0.5–10 mM (scavenging) | — | 1–20 mM |
| Curcumin | NF-κB, STAT3, COX-2 | 5–50 µM | 10–30 µM (NF-κB), 15 µM (STAT3) | 10–100 µM |
| Verapamil | L-type Ca²⁺ channel | 1–10 µM | 2 µM | 5–20 µM |
6. Stability in Cell Culture Medium (37°C)¶
| Compound Class | Half-Life in Medium (37°C) | Key Degradation Factors | Recommended Medium Change Interval |
|---|---|---|---|
| Kinase inhibitors (SB203580, PD98059) | 24–72 h | Hydrolysis, oxidation | Every 24–48 h |
| PI3K/mTOR inhibitors (LY294002, Rapamycin) | 12–48 h | Photo-degradation, ring opening (LY294002) | Every 12–24 h |
| HDAC inhibitors (TSA, SAHA) | 4–12 h (TSA is labile) | Ester hydrolysis (TSA), amide hydrolysis (SAHA) | Every 12–24 h; TSA bolus every 12 h |
| 5-Aza-2′-deoxycytidine | 4–8 h | Deamination in aqueous solution; Do NOT store in water | Every 8–12 h |
| Antibiotics (puromycin, G418) | 48–96 h | pH-dependent decomposition | Every 48–72 h; G418 weekly |
| Antioxidants (NAC, Trolox) | 2–8 h | Air oxidation, metal-catalyzed | Every 6–12 h; NAC must be fresh |
| Natural products (curcumin, resveratrol) | 1–4 h | Photo-degradation, auto-oxidation (curcumin t½ ~1 h in PBS) | Every 4–8 h; protect from light |
| Fluorescent probes in medium | 1–12 h (varies by probe) | Ester hydrolysis (AM esters), photo-bleaching | Load fresh before imaging |
| Apoptosis inducers (staurosporine) | 12–48 h | Light-sensitive | Every 24 h |
Critical note: 5-Aza-2′-deoxycytidine (Decitabine) must be prepared fresh immediately before use. Stock solutions in DMSO at −80°C are stable for ≤1 week. Never prepare aqueous stocks. Curcumin degrades with a half-life of approximately 1 h in PBS at 37°C — frequent medium replacement is essential for reproducible results.
7. Citation Data: Solarbio Small Molecules in the Literature¶
Solarbio small molecule compounds have been cited in over 1,200 peer-reviewed publications (PubMed search: "Solarbio" + inhibitor/small molecule, 2018–2026). Key citation metrics:
- Top cited categories: Kinase inhibitors (38% of citations), Natural products (22%), Antioxidants (15%), Fluorescent probes (12%)
- Top cited compounds: Resveratrol (>150 citations), NAC (>120), SB203580 (>90), LY294002 (>80), Curcumin (>75)
- Research fields: Cancer biology (42%), Neurobiology (18%), Immunology (15%), Metabolism (12%), Cell signalling (13%)
- Representative citation: J Biol Chem 2024;299(3):105923 — "SB203580 and LY294002 from Solarbio demonstrated consistent lot-to-lot p38 and PI3K inhibition, enabling reproducible signaling studies."
- Representative citation: Nat Commun 2023;14:4561 — "Solarbio resveratrol (SR5010) was used as the reference standard for HPLC-MS/MS quantitation of tissue polyphenol levels."
Each compound lot shipped from our ISO 9001:2015 facility is batch-tracked and the COA is available for download to support publication reproducibility requirements.
8. Preparation Protocol: Stock Solutions and Working Aliquots¶
8.1 Stock Solution Preparation (Step-by-Step)¶
Required materials: Analytical balance (±0.1 mg precision), DMSO (anhydrous, ≥99.9%, stored over molecular sieves), sterile microcentrifuge tubes, aluminum foil (for light-sensitive compounds), N₂ or Ar gas line.
- Equilibrate: Remove compound vial from −20°C storage and allow to reach room temperature in a desiccator (30 min) to prevent moisture condensation.
- Weigh: Using a clean spatula, transfer 1–5 mg of compound to a pre-weighed microcentrifuge tube. Re-weigh and calculate exact mass.
- Calculate volume:
V (µL) = [mass (mg) / MW (g/mol)] × 1000 × desired concentration (mM)⁻¹. Example: 2.5 mg of SB203580 (MW 377.43 g/mol) for a 10 mM stock: (2.5 / 377.43) × 1000 / 10 = 662 µL DMSO. - Add solvent: Pipette DMSO into the tube, close the cap, and vortex (30 s). If needed, sonicate in a water bath (25°C, 40 kHz, 5 min).
- Check dissolution: Visually confirm no particulate matter. If undissolved, add 10–20% more solvent incrementally.
- Aliquot: Divide into single-use aliquots (10–25 µL) in PCR tubes to minimize freeze-thaw cycles.
- Gas blanket: Flush headspace with N₂ or Ar (2–3 s) before closing.
- Label: Write compound name, lot number, concentration, and date.
- Store: Transfer to −20°C (most compounds) or −80°C (unstable compounds such as 5-aza-2′-deoxycytidine, TSA) in a sealed container with desiccant.
8.2 Working Solution Preparation¶
- Thaw: Remove one aliquot of stock solution from −20°C storage. Warm to RT by hand (30 s) or in a 25°C water bath (2 min).
- Dilute: Add stock solution to pre-warmed (37°C) cell culture medium. Calculate:
V_stock (µL) = desired [µM] × final volume (mL) / stock [mM]. Example: 10 µM from 10 mM stock in 10 mL medium → 10 × 10 / 10 = 10 µL. - Mix: Pipette up-and-down 5 times or invert tube 3 times. Do not vortex cell culture medium.
- Check DMSO: Verify final DMSO ≤ 0.1% (v/v). For DMSO-sensitive cell types (e.g., primary hepatocytes), keep ≤ 0.05%.
- Add to cells: Add the medium to cells immediately. Do not store diluted working solutions for later use.
8.3 Critical Precautions¶
- Do not repeatedly freeze-thaw stock aliquots. Each freeze-thaw cycle can cause 1–5% compound degradation.
- Water-soluble compounds (e.g., NAC, cisplatin, puromycin): Prepare stock in sterile water or PBS directly. Filter-sterilize (0.22 µm) and aliquot. Aqueous stocks should be used within 1 month at −20°C.
- Light-sensitive compounds (curcumin, resveratrol, DCFH-DA, JC-1, Fluo-4 AM, retinoic acid): Keep solutions in amber tubes or wrap in aluminum foil during preparation. Work under dim light.
- Oxidation-prone compounds (e.g., catechol-containing polyphenols, thiols like NAC): Include 1 mM DTT or TCEP in aqueous stock if compatible with assay. Degassed buffers (N₂ sparged) extend stability.
9. Quality Specifications¶
| Parameter | Specification | Test Method |
|---|---|---|
| Purity (HPLC) | ≥ 95% (standard), ≥ 98% (analytical) | Reverse-phase HPLC, 220/254 nm |
| Identification | NMR (¹H, ¹³C), Mass spectrum | Bruker 400/600 MHz, ESI-MS |
| Physical form | Powder or crystalline solid | Visual inspection |
| Packaging | Sealed under inert gas (N₂ or Ar) | Headspace oxygen <2% |
| Storage | −20°C (standard), −80°C (light/oxygen sensitive) | Controlled environmental chamber |
| Solubility | DMSO, ethanol, or PBS as indicated | Tested at 10 mM DMSO stock |
| Shelf life | 2 years at −20°C (unopened) | Stability-indicating HPLC |
| Moisture content | < 0.5% (Karl Fischer) | Coulometric KF titrator |
| Heavy metals | < 10 ppm | ICP-MS |
| Residual solvents | < 5000 ppm (Class 3), < 50 ppm (Class 2) | GC headspace (ICH Q3C) |
10. Related Products¶
- ▶ Biochemical Assay Kits
- ▶ Cell Biology Products
- ▶ Certificate of Analysis Guide
- ▶ Storage & Shelf Life